C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 473/16 (2006.01) A61K 31/52 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07D 473/40 (2006.01) C07D 519/00 (2006.01)
Patent
CA 2234609
2-Amino-6-anilino-purine derivatives of the formula I (see formula I) in which q is 1-5, R1 is halogen, lower alkyl, hydroxyl or lower alkanoyloxy; lower alkoxy which is unsubstituted or substituted by hydroxyl, lower alkoxy or carboxyl; a radical of the formula -O(-CH2-CH2-O)t-R6, in which t is 2-5 and R6 is hydrogen or lower alkyl; carboxyl, lower alkoxycarbonyl, piperazin-1-yl-carbonyl or carbamoyl; N-lower alkyl-carbamoyl, which is unsubstituted or substituted by hydroxyl or amino in the lower alkyl moiety; N,N-di-lower alkyl- carbamoyl, cyano, nitro, amino, lower alkanoylamino, lower alkylamino, N,N-di-lower alkylamino, aminosulfonyl or trifluoromethyl, where, if more than one radical R1 is present in the molecule, these can be identical to or different from one another, R2 is hydrogen, carbamoyl or N-lower alkyl-carbamoyl, m and n are each 0 or 1, where m is 0 if n is 1 and m is 1 if n is 0, R3 is lower alkyl or phenyl which are unsubstituted or in each case substituted by hydroxyl, lower alkoxy, amino, lower alkylamino or N,N-di-lower alkyl amino, and a) R4 is hydrogen, amino, phenylamino, lower alkylamino, hydroxyl, phenoxy, lower alkoxy, acyl having 1-30 C atoms, a substituted aliphatic hydrocarbon radical having not more than 29 C atoms, a carbocyclic radical having not more than 29 C atoms or a heterocyclic radical having not more than 20 C atoms and not more than 9 heteroatoms and R5 is amino, phenylamino, lower alkylamino, hydroxyl, phenoxy, lower alkoxy, acyl having 2-30 C atoms, a substituted aliphatic hydrocarbon radical having not more than 29 C atoms, a carbocyclic radical having not more than 29 C atoms or a heterocyclic radical having not more than 20 C atoms and not more than 9 heteroatoms, or b) R4 and R5 together are a substituted or unsubstituted alkylene or alkenylene radical having in each case not more than 15 C atoms, in which 1-3 C atoms can be replaced by oxygen, sulfur or nitrogen, and their salts are described. These compounds inhibit p34cdc2/cyclin Bcdc13 kinase and can be used for treatment of hyperproliferative diseases, for example tumour diseases.
On décrit des dérivés 2-amino-6-anilino-purines de la formule 1 dans laquelle les symboles sont tels que définis dans la revendication 1. Ces composés inhibent la p34<cdc2>/cycline B<cdc13> kinase et on peut les utiliser dans le traitement de maladies à hyperprolifération, par exemple des tumeurs.
Capraro Hans-Georg
Furet Pascal
Imbach Patricia
Zimmerman Jurg
Fetherstonhaugh & Co.
Novartis Ag
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